JP2013538214A5 - - Google Patents
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- Publication number
- JP2013538214A5 JP2013538214A5 JP2013526335A JP2013526335A JP2013538214A5 JP 2013538214 A5 JP2013538214 A5 JP 2013538214A5 JP 2013526335 A JP2013526335 A JP 2013526335A JP 2013526335 A JP2013526335 A JP 2013526335A JP 2013538214 A5 JP2013538214 A5 JP 2013538214A5
- Authority
- JP
- Japan
- Prior art keywords
- syk
- pharmaceutically acceptable
- osteoclasts
- optionally
- nasal
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 239000000203 mixture Substances 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000011780 sodium chloride Substances 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 210000000138 Mast Cells Anatomy 0.000 description 3
- 210000002997 Osteoclasts Anatomy 0.000 description 3
- 230000002148 osteoclast Effects 0.000 description 3
- 210000001331 Nose Anatomy 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 description 1
- 108040005185 1-phosphatidylinositol-3-kinase activity proteins Proteins 0.000 description 1
- 210000003651 Basophils Anatomy 0.000 description 1
- 208000006386 Bone Resorption Diseases 0.000 description 1
- 102100004646 LAT2 Human genes 0.000 description 1
- 101700015817 LAT2 Proteins 0.000 description 1
- 210000003928 Nasal Cavity Anatomy 0.000 description 1
- 229940100662 Nasal Drops Drugs 0.000 description 1
- 102000001332 SRC Human genes 0.000 description 1
- 101710009384 SRC Proteins 0.000 description 1
- 101700083924 VAV3 Proteins 0.000 description 1
- 230000024279 bone resorption Effects 0.000 description 1
- 210000004027 cells Anatomy 0.000 description 1
- 230000002596 correlated Effects 0.000 description 1
- 230000016396 cytokine production Effects 0.000 description 1
- 230000003436 cytoskeletal Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000001419 dependent Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000002257 embryonic structures Anatomy 0.000 description 1
- 102000006495 integrins Human genes 0.000 description 1
- 108010044426 integrins Proteins 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000003032 molecular docking Methods 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 230000000865 phosphorylative Effects 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 230000001105 regulatory Effects 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 230000000717 retained Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10008927.5 | 2010-08-27 | ||
| EP10008927 | 2010-08-27 | ||
| PCT/EP2011/003830 WO2012025186A1 (en) | 2010-08-27 | 2011-07-29 | Triazolopyrazine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013538214A JP2013538214A (ja) | 2013-10-10 |
| JP2013538214A5 true JP2013538214A5 (es) | 2015-07-16 |
| JP5951610B2 JP5951610B2 (ja) | 2016-07-13 |
Family
ID=44629489
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013526335A Expired - Fee Related JP5951610B2 (ja) | 2010-08-27 | 2011-07-29 | トリアゾロピラジン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9023851B2 (es) |
| EP (1) | EP2609098B1 (es) |
| JP (1) | JP5951610B2 (es) |
| KR (1) | KR20130110163A (es) |
| CN (1) | CN103068828B (es) |
| AR (1) | AR082726A1 (es) |
| AU (1) | AU2011295440B2 (es) |
| BR (1) | BR112013004517A2 (es) |
| CA (1) | CA2809331C (es) |
| EA (1) | EA201300282A1 (es) |
| ES (1) | ES2614128T3 (es) |
| IL (1) | IL224869A (es) |
| MX (1) | MX2013002198A (es) |
| SG (1) | SG188296A1 (es) |
| WO (1) | WO2012025186A1 (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013224421B2 (en) * | 2012-02-21 | 2017-03-02 | Merck Patent Gmbh | 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as Syk tryrosine kinase inhibitors and GCN2 serin kinase inhibitors |
| CN104159901B (zh) * | 2012-03-07 | 2016-10-26 | 默克专利股份公司 | 三唑并吡嗪衍生物 |
| EP2877598A1 (en) | 2012-07-24 | 2015-06-03 | Pharmacyclics, Inc. | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| CN104640850A (zh) * | 2012-10-26 | 2015-05-20 | 霍夫曼-拉罗奇有限公司 | 3,4-二取代的1h-吡唑和4,5-二取代的噻唑的syk抑制剂 |
| CN105026397B (zh) * | 2013-03-05 | 2017-06-30 | 默克专利股份公司 | 作为抗癌剂的9‑(芳基或杂芳基)‑2‑(吡唑基、吡咯烷基或环戊基)氨基嘌呤衍生物 |
| WO2014135244A1 (en) * | 2013-03-05 | 2014-09-12 | Merck Patent Gmbh | Triazolo[4,5-d]pyrimidine derivatives for the treatment of diseases such as cancer |
| WO2014180524A1 (en) * | 2013-05-06 | 2014-11-13 | Merck Patent Gmbh | Macrocycles as kinase inhibitors |
| US10821178B2 (en) | 2013-07-29 | 2020-11-03 | Board Of Regents Of The University Of Nebraska | Methods of treating biofilm infections comprising administering inhibitors of myeloid-derived suppressor cells |
| US9856263B2 (en) | 2014-04-28 | 2018-01-02 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine D1 ligands |
| KR101756934B1 (ko) | 2014-07-08 | 2017-07-12 | 연세대학교 산학협력단 | 피롤로[1,2-a]피라진 유도체, 이의 약학적으로 허용가능한 염, 이들 화합물의 제조방법 및 이를 유효성분으로 함유하는 골다공증 치료 또는 예방용 약학조성물 |
| CN110382508B (zh) | 2016-12-22 | 2022-08-02 | 卡里塞拉生物科学股份公司 | 用于抑制精氨酸酶活性的组合物和方法 |
| CR20200441A (es) | 2018-02-27 | 2021-03-15 | Incyte Corp | Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b |
| MX2020012376A (es) | 2018-05-18 | 2021-03-09 | Incyte Corp | Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b. |
| TW202402759A (zh) | 2018-07-05 | 2024-01-16 | 美商英塞特公司 | 作為a2a/a2b抑制劑之稠合吡嗪衍生物 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202202498A (zh) * | 2020-07-01 | 2022-01-16 | 大陸商四川海思科製藥有限公司 | 一種並環雜環衍生物及其在醫藥上的應用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2434871C2 (ru) * | 2005-02-03 | 2011-11-27 | Вертекс Фармасьютикалз Инкорпорейтед | Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы |
| JP4652906B2 (ja) * | 2005-06-30 | 2011-03-16 | 富士夫 宮脇 | 振動型マイクロインジェクション装置 |
| MX2008009557A (es) * | 2006-01-27 | 2009-01-07 | Shanghai Hengrui Pharm Co Ltd | Inhibidores de la cinasa de proteina de la pirrolo [3,2-c] piridin-4-ona-2-indolinona. |
| JP5180967B2 (ja) * | 2006-11-03 | 2013-04-10 | ブリストル−マイヤーズ スクイブ カンパニー | ピロロトリアジンキナーゼ阻害剤 |
| WO2008118823A2 (en) | 2007-03-26 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| VN29259A1 (en) | 2008-04-16 | 2012-04-25 | Portola Pharm Inc | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| WO2009155551A1 (en) | 2008-06-20 | 2009-12-23 | Genentech, Inc. | Triazolopyridine jak inhibitor compounds and methods |
| BRPI0909945A2 (pt) | 2008-06-20 | 2015-07-28 | Genentech Inc | "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase" |
| WO2010010188A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases. |
| WO2010010189A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | Novel compounds useful for the treatment of degenerative and inflammatory diseases |
| WO2010010184A1 (en) | 2008-07-25 | 2010-01-28 | Galapagos Nv | [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors |
| TWI453207B (zh) * | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| AU2010254806C1 (en) * | 2009-06-05 | 2016-07-07 | Cephalon, Inc. | Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives |
| US9145399B2 (en) * | 2010-01-15 | 2015-09-29 | Janssen Pharmaceuticals, Inc. | Substituted bicyclic triazole derivatives as gamma secretase modulators |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
-
2011
- 2011-07-29 ES ES11738630.0T patent/ES2614128T3/es active Active
- 2011-07-29 WO PCT/EP2011/003830 patent/WO2012025186A1/en active Application Filing
- 2011-07-29 BR BR112013004517A patent/BR112013004517A2/pt not_active Application Discontinuation
- 2011-07-29 US US13/819,120 patent/US9023851B2/en active Active
- 2011-07-29 EP EP11738630.0A patent/EP2609098B1/en not_active Not-in-force
- 2011-07-29 KR KR20137007843A patent/KR20130110163A/ko not_active Application Discontinuation
- 2011-07-29 JP JP2013526335A patent/JP5951610B2/ja not_active Expired - Fee Related
- 2011-07-29 EA EA201300282A patent/EA201300282A1/ru unknown
- 2011-07-29 MX MX2013002198A patent/MX2013002198A/es not_active Application Discontinuation
- 2011-07-29 AU AU2011295440A patent/AU2011295440B2/en not_active Ceased
- 2011-07-29 SG SG2013014006A patent/SG188296A1/en unknown
- 2011-07-29 CA CA2809331A patent/CA2809331C/en not_active Expired - Fee Related
- 2011-07-29 CN CN201180041643.5A patent/CN103068828B/zh not_active Expired - Fee Related
- 2011-08-26 AR ARP110103111 patent/AR082726A1/es unknown
-
2013
- 2013-02-21 IL IL224869A patent/IL224869A/en not_active IP Right Cessation
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